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Assay Detail

CHEMBL3801663

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.
Zou MF, Keck TM, Kumar V, Donthamsetti P, Michino M, Burzynski C, Schweppe C, Bonifazi A, Free RB, Sibley DR, Janowsky A, Shi L, Javitch JA, Newman AH.
J Med Chem (2016) 59 : 2973 -2988
PubMed 27035329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.58 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285755 1 8.76
CHEMBL3797209 1 8.22
CHEMBL3798803 1 7.99
CHEMBL240773 QUINPIROLE 2.0 1 7.53
CHEMBL3800165 1 7.32
CHEMBL3799157 1 6.73
CHEMBL3797740 1 6.54
CHEMBL59 DOPAMINE 4.0 1 6.53
CHEMBL3798179 1 6.47
CHEMBL434665 1 6.39
CHEMBL3799626 1 5.96
CHEMBL3800633 1 5.58
CHEMBL419792 SUMANIROLE 3.0 1 5.20
CHEMBL3799271 1 4.93
CHEMBL3798018 1 4.57
CHEMBL26181 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285755 Ki = 1.75 nM 8.76
CHEMBL3797209 Ki = 6.05 nM 8.22
CHEMBL3798803 Ki = 10.3 nM 7.99
CHEMBL240773 QUINPIROLE Ki = 29.3 nM 7.53
CHEMBL3800165 Ki = 47.9 nM 7.32
CHEMBL3799157 Ki = 187.0 nM 6.73
CHEMBL3797740 Ki = 290.0 nM 6.54
CHEMBL59 DOPAMINE Ki = 293.0 nM 6.53
CHEMBL3798179 Ki = 337.0 nM 6.47
CHEMBL434665 Ki = 410.0 nM 6.39
CHEMBL3799626 Ki = 1090.0 nM 5.96
CHEMBL3800633 Ki = 2610.0 nM 5.58
CHEMBL419792 SUMANIROLE Ki = 6330.0 nM 5.20
CHEMBL3799271 Ki = 11800.0 nM 4.93
CHEMBL3798018 Ki = 27200.0 nM 4.57
CHEMBL26181 Ki - -